RU2328308C2 - Комбинирование ингибиторов fbp-азы и антидиабетических средств для лечения диабета - Google Patents
Комбинирование ингибиторов fbp-азы и антидиабетических средств для лечения диабета Download PDFInfo
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- RU2328308C2 RU2328308C2 RU2003103436/15A RU2003103436A RU2328308C2 RU 2328308 C2 RU2328308 C2 RU 2328308C2 RU 2003103436/15 A RU2003103436/15 A RU 2003103436/15A RU 2003103436 A RU2003103436 A RU 2003103436A RU 2328308 C2 RU2328308 C2 RU 2328308C2
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- Prior art keywords
- alkyl
- aryl
- group
- aralkyl
- alicyclic
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- 239000003112 inhibitor Substances 0.000 title claims abstract description 97
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- 229940125708 antidiabetic agent Drugs 0.000 title claims description 45
- 230000003914 insulin secretion Effects 0.000 claims abstract description 44
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 42
- 239000000203 mixture Substances 0.000 claims abstract description 26
- 230000000694 effects Effects 0.000 claims abstract description 14
- 230000002265 prevention Effects 0.000 claims abstract 8
- 125000000217 alkyl group Chemical group 0.000 claims description 628
- 125000003118 aryl group Chemical group 0.000 claims description 609
- 125000004122 cyclic group Chemical group 0.000 claims description 326
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 311
- 125000002723 alicyclic group Chemical group 0.000 claims description 297
- 125000001072 heteroaryl group Chemical group 0.000 claims description 237
- 125000004429 atom Chemical group 0.000 claims description 201
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- 125000004093 cyano group Chemical group *C#N 0.000 claims description 118
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- 229910052717 sulfur Inorganic materials 0.000 claims description 106
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- 229910052757 nitrogen Inorganic materials 0.000 claims description 92
- PXBRQCKWGAHEHS-UHFFFAOYSA-N dichlorodifluoromethane Chemical compound FC(F)(Cl)Cl PXBRQCKWGAHEHS-UHFFFAOYSA-N 0.000 claims description 90
- 125000003342 alkenyl group Chemical group 0.000 claims description 84
- 229910052799 carbon Inorganic materials 0.000 claims description 78
- PIGFYZPCRLYGLF-UHFFFAOYSA-N Aluminum nitride Chemical compound [Al]#N PIGFYZPCRLYGLF-UHFFFAOYSA-N 0.000 claims description 66
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- 101710109119 Fructose-1,6-bisphosphatase, cytosolic Proteins 0.000 claims description 64
- 101710198902 Fructose-1,6-bisphosphate aldolase/phosphatase Proteins 0.000 claims description 64
- 229910052739 hydrogen Inorganic materials 0.000 claims description 63
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 62
- 229910052698 phosphorus Inorganic materials 0.000 claims description 62
- 229940002612 prodrug Drugs 0.000 claims description 59
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- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims description 57
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- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 48
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- ZRALSGWEFCBTJO-UHFFFAOYSA-N Guanidine Chemical compound NC(N)=N ZRALSGWEFCBTJO-UHFFFAOYSA-N 0.000 claims description 42
- 125000002947 alkylene group Chemical group 0.000 claims description 40
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- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 37
- OAICVXFJPJFONN-UHFFFAOYSA-N Phosphorus Chemical compound [P] OAICVXFJPJFONN-UHFFFAOYSA-N 0.000 claims description 36
- 239000011574 phosphorus Substances 0.000 claims description 36
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 35
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- 125000000623 heterocyclic group Chemical group 0.000 claims description 34
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- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 19
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- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 19
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- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims description 17
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- XZWYZXLIPXDOLR-UHFFFAOYSA-N metformin Chemical compound CN(C)C(=N)NC(N)=N XZWYZXLIPXDOLR-UHFFFAOYSA-N 0.000 claims description 8
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- XUFXOAAUWZOOIT-SXARVLRPSA-N (2R,3R,4R,5S,6R)-5-[[(2R,3R,4R,5S,6R)-5-[[(2R,3R,4S,5S,6R)-3,4-dihydroxy-6-methyl-5-[[(1S,4R,5S,6S)-4,5,6-trihydroxy-3-(hydroxymethyl)-1-cyclohex-2-enyl]amino]-2-oxanyl]oxy]-3,4-dihydroxy-6-(hydroxymethyl)-2-oxanyl]oxy]-6-(hydroxymethyl)oxane-2,3,4-triol Chemical group O([C@H]1O[C@H](CO)[C@H]([C@@H]([C@H]1O)O)O[C@H]1O[C@@H]([C@H]([C@H](O)[C@H]1O)N[C@@H]1[C@@H]([C@@H](O)[C@H](O)C(CO)=C1)O)C)[C@@H]1[C@@H](CO)O[C@@H](O)[C@H](O)[C@H]1O XUFXOAAUWZOOIT-SXARVLRPSA-N 0.000 claims description 6
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Classifications
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/66—Phosphorus compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/426—1,3-Thiazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
- A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
Landscapes
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Diabetes (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Endocrinology (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Emergency Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US21653100P | 2000-07-06 | 2000-07-06 | |
| US60/216,531 | 2000-07-06 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2003103436A RU2003103436A (ru) | 2004-06-27 |
| RU2328308C2 true RU2328308C2 (ru) | 2008-07-10 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2003103436/15A RU2328308C2 (ru) | 2000-07-06 | 2001-07-05 | Комбинирование ингибиторов fbp-азы и антидиабетических средств для лечения диабета |
Country Status (18)
| Country | Link |
|---|---|
| EP (1) | EP1372660A2 (fr) |
| JP (1) | JP2004508297A (fr) |
| KR (1) | KR100854851B1 (fr) |
| CN (2) | CN101301294A (fr) |
| AU (2) | AU7327101A (fr) |
| BR (1) | BR0112212A (fr) |
| CA (1) | CA2412142A1 (fr) |
| CZ (1) | CZ20035A3 (fr) |
| HU (1) | HUP0301830A3 (fr) |
| IL (2) | IL153513A0 (fr) |
| MX (1) | MXPA02012713A (fr) |
| NO (1) | NO20030034L (fr) |
| NZ (1) | NZ523227A (fr) |
| PL (1) | PL365779A1 (fr) |
| RU (1) | RU2328308C2 (fr) |
| SK (1) | SK62003A3 (fr) |
| WO (1) | WO2002003978A2 (fr) |
| ZA (1) | ZA200300044B (fr) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2664422C2 (ru) * | 2012-10-08 | 2018-08-17 | ЭлДжи КЕМ, ЛТД. | Комбинированный препарат, содержащий гемиглиптин и метформин, и способ его получения |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7048906B2 (en) | 1995-05-17 | 2006-05-23 | Cedars-Sinai Medical Center | Methods of diagnosing and treating small intestinal bacterial overgrowth (SIBO) and SIBO-related conditions |
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| TW200738245A (en) * | 2005-08-22 | 2007-10-16 | Sankyo Co | Pharmaceutical composition containing FBPase inhibitor |
| WO2007129522A1 (fr) * | 2006-04-10 | 2007-11-15 | Daiichi Sankyo Company, Limited | Préparation obtenue par voie sèche |
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| CN107312039B (zh) | 2012-08-30 | 2019-06-25 | 江苏豪森药业集团有限公司 | 一种替诺福韦前药的制备方法 |
| CN104788350A (zh) * | 2014-01-22 | 2015-07-22 | 天津大学 | 一种通过快速冷却结晶法获得甲糖宁药用优势晶型的方法 |
| CN106831437B (zh) * | 2016-02-03 | 2019-06-21 | 华中师范大学 | 含硝基乙烯基的酯类化合物及其制备方法和应用 |
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- 2001-07-05 PL PL01365779A patent/PL365779A1/xx unknown
- 2001-07-05 AU AU7327101A patent/AU7327101A/xx active Pending
- 2001-07-05 KR KR1020037000126A patent/KR100854851B1/ko not_active Expired - Fee Related
- 2001-07-05 NZ NZ523227A patent/NZ523227A/en not_active IP Right Cessation
- 2001-07-05 CA CA002412142A patent/CA2412142A1/fr not_active Abandoned
- 2001-07-05 CN CNA200810098112XA patent/CN101301294A/zh active Pending
- 2001-07-05 CZ CZ20035A patent/CZ20035A3/cs unknown
- 2001-07-05 HU HU0301830A patent/HUP0301830A3/hu unknown
- 2001-07-05 IL IL15351301A patent/IL153513A0/xx unknown
- 2001-07-05 AU AU2001273271A patent/AU2001273271B2/en not_active Ceased
- 2001-07-05 MX MXPA02012713A patent/MXPA02012713A/es not_active Application Discontinuation
- 2001-07-05 BR BR0112212-6A patent/BR0112212A/pt not_active IP Right Cessation
- 2001-07-05 SK SK6-2003A patent/SK62003A3/sk unknown
- 2001-07-05 CN CNB018149243A patent/CN100396283C/zh not_active Expired - Fee Related
- 2001-07-05 EP EP01952530A patent/EP1372660A2/fr not_active Withdrawn
- 2001-07-05 JP JP2002508433A patent/JP2004508297A/ja active Pending
- 2001-07-05 RU RU2003103436/15A patent/RU2328308C2/ru not_active IP Right Cessation
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2002
- 2002-12-18 IL IL153513A patent/IL153513A/en not_active IP Right Cessation
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2003
- 2003-01-02 ZA ZA200300044A patent/ZA200300044B/en unknown
- 2003-01-03 NO NO20030034A patent/NO20030034L/no not_active Application Discontinuation
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| WO1998039343A1 (fr) * | 1997-03-07 | 1998-09-11 | Metabasis Therapeutics, Inc. | Nouveaux inhibiteurs de benzimidazole de fructose-1,6-bisphosphatase |
| WO1999047549A1 (fr) * | 1998-03-16 | 1999-09-23 | Ontogen Corporation | Piperazines utilisees en tant qu'inhibiteurs de fructose-1,6-bisphosphatase (fbpase) |
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| RU2664422C2 (ru) * | 2012-10-08 | 2018-08-17 | ЭлДжи КЕМ, ЛТД. | Комбинированный препарат, содержащий гемиглиптин и метформин, и способ его получения |
Also Published As
| Publication number | Publication date |
|---|---|
| NO20030034L (no) | 2003-03-05 |
| KR20030031952A (ko) | 2003-04-23 |
| EP1372660A2 (fr) | 2004-01-02 |
| WO2002003978A3 (fr) | 2003-10-16 |
| SK62003A3 (en) | 2003-09-11 |
| IL153513A (en) | 2014-07-31 |
| HUP0301830A2 (hu) | 2003-11-28 |
| IL153513A0 (en) | 2003-07-06 |
| AU7327101A (en) | 2002-01-21 |
| MXPA02012713A (es) | 2004-09-10 |
| CN101301294A (zh) | 2008-11-12 |
| PL365779A1 (en) | 2005-01-10 |
| WO2002003978A2 (fr) | 2002-01-17 |
| JP2004508297A (ja) | 2004-03-18 |
| ZA200300044B (en) | 2004-05-06 |
| CN100396283C (zh) | 2008-06-25 |
| KR100854851B1 (ko) | 2008-08-27 |
| CN1599612A (zh) | 2005-03-23 |
| CA2412142A1 (fr) | 2002-01-17 |
| NZ523227A (en) | 2005-04-29 |
| BR0112212A (pt) | 2003-12-30 |
| AU2001273271B2 (en) | 2006-01-05 |
| CZ20035A3 (cs) | 2003-05-14 |
| NO20030034D0 (no) | 2003-01-03 |
| HUP0301830A3 (en) | 2007-10-29 |
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